Related Products of 2106-04-9, These common heterocyclic compound, 2106-04-9, name is 3-Chloro-2-fluoroaniline, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Step 1 .2: Ethyl-5-((3-chloro-2-fluorophenylamino)(4-chlorophenyl)methyl)-1-isopropyl-2-(2- methoxyphenyl)-1 H-imidazole-4-carboxylate 3-chloro-2-fluoroaniline (90 mg, 0.621 mmol) was added to a solution of the product of step 1.3 (242 mg, 0.477 mmol) in dioxane (5 ml) and stirred at 60C over night. 3-Chloro- 2-fluoroaniline (90 mg, 0.621 mmol) was added again to the reaction mixture and heated at 100C for 3 hr. The solution was diluted with EtOAc and washed twice with a 5% aqueous citric acid solution. The water phase was back extracted with EtOAc and the combined organic layers were washed with saturated aqueous NaHC03, dried over Na2S04 and evaporated to afford 800 mg of brown oil. The residue was purified by preparative HPLC (Waters xBridge (30 / 100 mm), 0.1 % TFA-water/0.1 % TFA-acetonitrile; gradient acetonitrile 30 to 60% in 10 min, then 5 min at 60%, 60 – 90% in 10 min and 2 min at 100%) to afford 176 mg (0.313 mmol, 65.6% yield) of the title compound. LCMS: (M+H) = 556/557; tR = 1 .46 min (LC-MS 3). HPLC: tR = 5.35 min (H PLC 2) 1 H-NMR (MeOD, 600.13 MHz) delta ppm 7.52 (t, 1 H) 7.39-7.30 (m, 5H) 7.12 (m, 1 H) 7.07 (t, 1 H) 6.96 (t, 1 H) 6.86 (t, 1 H) 6.77 (t, 1 H) 6.72-6.30 (m, 1 H) 4.37 (quin, 1 H) 4.27 (q, 2H) 3.77 (s, 3H) 1 .31 -1.05 (m, 9H)
The synthetic route of 2106-04-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; NOVARTIS AG; FURET, Pascal; GUAGNANO, Vito; HOLZER, Philipp; KALLEN, Joerg; MAH, Robert; MASUYA, Keiichi; SCHLAPBACH, Achim; VAUPEL, Andrea; WO2014/115077; (2014); A1;,
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